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Protected lactam-bridged dipeptides for use as conformational constraints in peptides

RM Freidinger, DS Perlow…

文献索引:Freidinger, Roger M.; Perlow, Debra Schwenk; Veber, Daniel F. Journal of Organic Chemistry, 1982 , vol. 47, # 1 p. 104 - 109

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被引用次数: 239

摘要

General methods have been devised for the synthesis of lactam-constrained dipeptide analogues having five-, six-, and seven-membered rings. Three different paths from protected chiral a-amino acids to lactams involving intramolecular alkylation, intramolecular acylation, and insertion of a one carbon unit by condensation with formaldehyde have been utilized. The first two methods produce chiral products stereospecifically, but considerable ...